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dexamethasone (OT502 / IBI10090 / OT 502)

✓ Approved

Ocumension Therapeutics Co., Ltd. · NR3C1 · 类固醇

什么是 dexamethasone？

dexamethasone 是一种类固醇，由Ocumension Therapeutics Co., Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intraocular Injection。

药物档案

商品名OT502, IBI10090, OT 502
公司Ocumension Therapeutics Co., Ltd.
药物类别类固醇, 小分子
分子靶点NR3C1
给药途径Injectable (Others), Intraocular Injection
状态Approved
来源： ClinicalTrials.gov, Ocumension Therapeutics Co., Ltd.

作用机制

分子靶点

dexamethasone 作用于 1 个分子靶点：

NR3C1nuclear receptor subfamily 3 group C member 1 (GR, GCCR)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

dexamethasone 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Eye disordersCataract✓ Approved

相关研究文献

PubMedKnee surgery & related research2026-08-04

Optimizing perioperative systemic dexamethasone use in total knee arthroplasty: a narrative review on current evidence.

Park Jisu J, Kim Tae Woo TW, Chang Moon Jong MJ, Kang Seung-Baik SB

Perioperative corticosteroids, particularly dexamethasone, have become a widely adopted component of multimodal pain management in total knee arthroplasty (TKA). While clinical practice guidelines strongly recommend their use, detailed guidance on optimal dosing, frequency, and safety in special populations, especially patients with diabetes mellitus, is still limited. This narrative review synthesizes the current evidence on systemic perioperative dexamethasone use in TKA, focusing on clinical questions: agent and route selection, dose optimization, dosing frequency, and safety, including considerations for patients with diabetes. A literature search of PubMed, EMBASE, and the Cochrane Library was conducted for studies published between January 2015 and April 2026. Randomized controlled trials, systematic reviews, meta-analyses, clinical practice guidelines, and observational studies addressing systemic corticosteroid use in primary TKA were included. Recent evidence supports intravenous (IV) dexamethasone as the most commonly studied and clinically practical systemic agent. A 16 mg dose provides greater early analgesic and antiemetic benefit than lower doses, and repeat dosing through postoperative day (POD) 1 is supported, with extension to POD 2 emerging but not yet definitive. Perioperative dexamethasone has not been associated with increased infection or wound complications. In patients with well-controlled diabetes, it appears safe with appropriate glycemic monitoring, although safety data are largely limited to doses of 8-10 mg. Current evidence supports IV dexamethasone as an effective component of multimodal analgesia after TKA. In the general TKA population, 16 mg appears more effective than lower doses for early postoperative pain, opioid consumption, and postoperative nausea and vomiting (PONV)-related outcomes. Repeat dosing through POD 1 is supported by available evidence, whereas extension to POD 2 remains promising but requires further validation. In patients with well-controlled diabetes, perioperative dexamethasone appears safe with appropriate glycemic monitoring, although safety data are largely limited to doses of 8-10 mg, and the safety of the 16 mg dose in this population remains insufficiently defined.

PMID 42547910
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PubMedBeyoglu eye journal2026-08-04

Comparison of Patients with Diabetic Macular Edema Undergoing Early versus Late Switch from Intravitreal Anti-VEGF Therapy to Dexamethasone Implant.

Yildiz Dilan D, Aday Oznur O, Cakir Akin A, Karatas Gamze G et al.

To compare anatomical and functional outcomes in patients with diabetic macular edema who exhibited a suboptimal response to intravitreal anti-VEGF therapy and underwent early (<6 months) versus late (≥6 months) switch to an intravitreal dexamethasone implant. This retrospective comparative study included 141 eyes of 141 patients with diabetic macular edema. Patients received at least three consecutive anti-VEGF injections without adequate anatomical or functional response and were subsequently switched to a dexamethasone implant. Patients were divided into two groups: early switch (<6 months) and late switch (≥6 months). Best-corrected visual acuity, central macular thickness, optical coherence tomography biomarkers, intraocular pressure, lens status, number of injections, and complications were analyzed. Of 141 patients (79 females, 62 males; mean age 65.3±8.9 years), 49 were in the early switch group and 92 were in the late switch group. At baseline, best-corrected visual acuity was marginally better in the late switch group (p=0.049), while baseline central subfield thickness was comparable (p=0.35). After switching, both groups showed a significant reduction in central subfield thickness (p<0.01), with no difference between the groups (p=0.58). Best-corrected visual acuity improved significantly in both groups; however, visual gain was greater in the early switch group (p=0.038). The mean number of total intravitreal injections was significantly higher in the late switch group (p<0.01). Mean intraocular pressure increased from 16.3 to 18.0 mmHg in both groups (p<0.01), with no intergroup difference. Thirty-one patients required cataract surgery during follow-up, without correlation with switch timing. Optical coherence tomography biomarkers revealed that patients with ellipsoid zone disruption had poorer BCVA outcomes, while those with subfoveal serous detachment exhibited greater central subfield thickness reduction (p<0.05). Early switch from anti-VEGF to a dexamethasone implant in refractory diabetic macular edema provides superior functional outcomes and reduces treatment burden compared with late switch, despite similar anatomical improvements.

PMID 42549215
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PubMedPain physician2026-08-04

Prolonging Peripheral Nerve Blocks in Adults: A Narrative Review of Adjunct Medications for Single-Injection Techniques.

Jha Sachin Sunny SS

Single-injection peripheral nerve blocks (PNBs) are a cornerstone of multimodal perioperative analgesia. However, the duration of commonly used long-acting local anesthetics is finite; many patients experience abrupt and sometimes severe "rebound pain" as the block resolves. This phenomenon is particularly prominent after painful orthopedic procedures and may increase early opioid consumption and reduce patient satisfaction. To review the effectiveness and safety of pharmacologic adjuncts used to prolong adult single-injection PNBs and to provide practical, clinically oriented recommendations for their use. Narrative review. I conducted a focused narrative review of randomized controlled trials, observational studies, and systematic reviews or meta-analyses evaluating adjunct medications administered with single-injection PNBs in adults. The agents considered were dexamethasone, dexmedetomidine, clonidine, morphine, fentanyl, buprenorphine, magnesium sulfate, midazolam, and ketamine. The outcomes of interest were sensory block duration and analgesia, postoperative opioid consumption, rebound pain, and adverse events. Dexamethasone, given intravenously or perineurally, consistently prolongs analgesia by approximately 6-8 hours and reduces early opioid use. Buprenorphine, administered perineurally, often extends analgesia to 24-48 hours but increases postoperative nausea. Dexmedetomidine modestly prolongs a block's duration and improves a block's quality, but is associated with dose-dependent bradycardia, hypotension, and sedation. Clonidine yields smaller gains in a block's duration with similar hemodynamic and sedative concerns to dexmedetomidine. Magnesium sulfate and midazolam produce modest and more variable benefits. Ketamine has inconsistent effects on a block's duration but may help mitigate hyperalgesia in select patients. Conventional opioids (morphine, fentanyl) provide little incremental benefit as perineural adjuncts; they also increase opioid-typical adverse effects. This is a narrative rather than a systematic review; heterogeneity among studies in block type, local anesthetic formulation, dosing, and outcome definitions precludes pooled quantitative estimates. Dexamethasone and buprenorphine have the strongest and most consistent evidence for clinically meaningful prolongation of single-injection PNBs in adults and may be considered first-line adjuncts in appropriate patients. Dexmedetomidine, clonidine, magnesium, midazolam, and ketamine may be useful in some situations when their specific benefit-risk profiles are acceptable. Conventional opioids offer little advantage as perineural adjuncts and are not recommended for routine use. Evidence-based selection of adjuncts within a multimodal analgesic strategy can improve postoperative analgesia, reduce opioid exposure, and potentially attenuate rebound pain.

PMID 42550518
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PubMedPain physician2026-08-04

Safety and Effectiveness of Different Approaches for Epidural Steroid Injections in Lumbar Spinal Stenosis: A Systematic Review and Meta-Analysis.

Wilderman Igor I, Sarzetto Francesca F, Didari Tina T, Manor Rotem Frish RF et al.

Lumbar canal stenosis is a common degenerative disorder that causes pain and functional alterations. Epidural steroid injections (ESIs) are often used to treat the symptoms of this condition; however, treatment protocols can vary significantly, and no standardized practice for the management of lumbar canal stenosis has been established. To identify the optimal method of administration for maximizing the effectiveness and duration of pain relief and functionality improvements provided by ESIs. Systematic review and meta-analysis. We searched PubMed, Google Scholar, ScienceDirect, CINAHL, EMBASE, and OVID for clinical trials published from January 2000 to December 2025 that examined the effectiveness of different ESI protocols to ameliorate pain and functionality in spinal stenosis patients. The search terms included ("lumbar spinal stenosis" OR "lumbar canal stenosis" or "lumbar foraminal stenosis") AND "epidural steroid/corticosteroid injection(s)" AND ("interlaminar" OR "caudal" OR "transforaminal" OR "route"). Studies that met exclusion criteria were those that did not use human patients, that were not focused on lumbar stenosis, that had no consistent protocol, or did not express their outcomes as decreases in pain intensity. The risk of bias was assessed with the Cochrane RoB2 tool. We conducted a meta-analysis on the data from individual groups extracted from different studies, including sub-group and meta-regression analyses, to identify variables with significant effects. In total, 33 groups (comprising 1,350 patients) were extracted from 24 studies, with results from one week to 12 months after the injection. Most studies reported significant pain relief up to 3 months from the injections, and some reported that such pain relief persisted even after a year. Of all the factors that influenced the results, the type of steroid used had the greatest effect, with betamethasone providing the greatest and more prolonged relief. Triamcinolone and methylprednisolone offered similar initial levels of pain relief, though it decreased more rapidly, whereas dexamethasone showed the lowest level of benefits. Moreover, the pain relief effect was significantly weaker in patients with severe stenosis, and functionality improvements were also limited in patients with moderate/severe stenosis. In contrast, route of administration (transforaminal, interlaminar, or caudal), dose size, and other parameters showed no significant differences. Most groups included in the analysis were small, with 22 of the 33 (66.7%) having fewer than 50 patients, and only one group including more than 100. Furthermore, the results overall were significantly heterogeneous, and the follow-up times varied, meaning that some subgroups had only one result or none whatsoever at certain time points and limiting the subgroup analysis. ESIs are an effective treatment for the pain caused by spinal stenosis; betamethasone, even at a low dose, appears to provide the greatest benefits, whereas dexamethasone seems the least effective. Patients with mild or moderate stenosis are more likely to experience positive results from ESIs, and the administration route can be chosen depending on the patient's status, offering similar effects. The transforaminal route is likely more beneficial in single-level stenosis, while interlaminar (at the level of maximal stenosis or one caudad) and caudal injections are more appropriate for multilevel pathologies.

PMID 42550520
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PubMedBeyoglu eye journal2026-08-04

Efficacy and Safety of Intravitreal Triamcinolone Acetonide Alone or Combined with Intravitreal Bevacizumab in the Treatment of Macular Edema Secondary to Branch Retinal Vein Occlusion.

Diracoglu Aynur A, Agin Abdullah A, Cakir Mehmet M, Demirok Ahmet A

To compare the efficacy and safety of intravitreal triamcinolone acetonide (IVTA) monotherapy versus combined intravitreal triamcinolone acetonide and bevacizumab (IVTA+IVB) therapy in the treatment of macular edema secondary to branch retinal vein occlusion (BRVO). In this retrospective study, 66 eyes of 65 patients with BRVO-related macular edema were evaluated. Patients were divided into two groups: IVTA monotherapy (n=37) and IVTA+IVB combination therapy (n=29). Central macular thickness (CMT), best-corrected visual acuity (BCVA), and intraocular pressure (IOP) were measured at baseline, week 1, and months 1, 3, and 6 after injection. Both groups demonstrated significant improvements in BCVA and reductions in CMT compared with baseline (p<0.001), with no statistically significant differences between the groups at any follow-up time point. IOP was significantly elevated in the IVTA group at several time points (p<0.05), while the combination group showed stable IOP levels. New-onset glaucoma developed in 8 patients in the IVTA group and only 1 patient in the combination group. No serious ocular complications occurred in either group. Both treatment regimens provided comparable anatomical and visual improvements; however, combination therapy was associated with a more favorable safety profile. Although the use of IVTA has declined in contemporary clinical practice in favor of intravitreal dexamethasone implants, this study suggests that IVTA alone or in combination may still offer a viable and cost-effective alternative in regions where access to current therapies is limited or in low-resource settings.

PMID 42549240
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PubMedJournal of ethnopharmacology2026-08-04

Xiaoqinglong Decoction Suppresses M1 Macrophage Polarization in COPD via the MET/AKT/HK2 Axis: An Integrated Multi-Omics Analysis.

Zhang Furong F, Gu Jingzhe J, Li Yujing Y, Zhang Yao Y et al.

Xiaoqinglong Decoction (XQLD), a classic herbal formula for respiratory diseases, is clinically effective against chronic obstructive pulmonary disease (COPD). However, whether its anti-inflammatory effects involve modulation of macrophage immunometabolism remains unknown. This study investigated whether XQLD suppresses M1 macrophage polarization in COPD by modulating glycolysis-related pathways. COPD was induced in rats by alternate intratracheal instillation of papain (Papa) and lipopolysaccharide (LPS). After modeling, the rats received XQLD at high, medium, and low doses, while a separate group received dexamethasone as the positive control. Therapeutic effects on pulmonary function and lung pathology were evaluated, along with M1 polarization by immunofluorescence and other assays. Core pathways were identified through transcriptomic-metabolomic integration. In vitro, XQLD-containing serum was used to treat THP-1-derived M1 macrophages, and M1 polarization, glycolytic indicators, and MET/AKT/HK2 pathway proteins were assessed following treatment with 2-DG, HK2 overexpression, or HGF. XQLD dose-dependently improved pulmonary function and lung pathology, and reduced M1 infiltration. Multi-omics identified MET and HK as central nodes; XQLD reversed aberrant MET/AKT/HK2 expression in vivo. In vitro, XQLD-containing serum inhibited M1 polarization, glycolytic flux, and HGF-induced MET/AKT/HK2 signaling, with its effects partially reversed by HK2 overexpression. XQLD attenuates M1 macrophage-driven airway inflammation by normalizing the MET/AKT/HK2 signaling-metabolic axis and suppressing, at least in part, HK2-dependent glycolysis. These findings provide a novel immunometabolic mechanism for the traditional anti-inflammatory efficacy of XQLD in COPD.

PMID 42546823
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